摘要 |
Compounds are described of general formula (I) and salts and solvates thereof, including physiologically acceptable salts and solvates thereof, in which: Z represents either Het, (a), or (b); Het represents an optionally substituted bicyclic or tricyclic ring selected from quinolin-4-yl, isoquinolin-1-yl, isoquinolin-3-yl, quinolin-3-yl, quinolin-2-yl, quinoxalin-2-yl, naphthalen-1-yl, naphthalen-2-yl, indol-2-yl, 4-oxo-4H-1-benzopyran-2-yl, phenazin-1-yl and phenothiazin-1-yl or an aryl substituted monocyclic ring selected from 2-aryl-4-thiazolyl, 2-aryl-5-thiazolyl, 5-aryl-2-thienyl, 2-aryl-4-triazolyl and 1-aryl-4-pyrazolyl where aryl represents a phenyl or pyridyl ring optionally substituted by a halogen atom or a trifluoromethyl, C1-4 alkyl or C1-4 alkoxy group. The above-mentioned bicyclic or tricyclic rings may be unsubstituted or substituted by one, two or three groups selected from C1-4 alkyl and C1-4 alkoxy. Quinolin-4-yl rings may also be substituted in the ring 2 position by phenyl or phenyl substituted by C1-4 alkoxy. Indol-2-yl rings may also be substituted in the ring 3 position by benzoyl; R8 represents a hydrogen or halogen atom or a C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, amino or nitro group; p represent 1; or when R8 represents C1-4 alkoxy p may also represent 2 or 3; R9 represents a hydrogen or halogen atom or a C1-4 alkyl, C1-4 alkoxy or C1-4 alkylthio group; R10 and R11 may each represent a hydrogen atom or together form a bond or a linking atom selected from -O- or -S-; and X represents an oxygen atom or NR12 (where R12 represents a hydrogen atom or a C1-4 alkyl group). The novel compounds of formula (I) can sensitize multi-drug resistant cancer cells to chemotherapeutic agents and may be formulated for use in therapy, particularly to improve or increase the efficacy of an anti-tumour drug. |
申请人 |
LABORATOIRES GLAXO S.A. |
发明人 |
DUMAITRE, BERNARD, ANDRE;DODIC, NERINA;DAUGAN, ALAIN, CLAUDE-MARIE;PIANETTI, PASCAL, MAURICE, CHARLES |